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Trastuzumab is a therapeutic humanised monoclonal antibody targeting the Her2 receptor tyrosine kinase. Her2 is over-expressed, due to gene amplification, in approximately 30% of breast cancers and confers a worse prognosis. Trastuzumab has been used clinically for over a decade and is now used routinely in the treatment of Her2-positive breast cancer in the metastatic and adjuvant setting. Its mechanisms of action and resistance, as well as its pharmacokinetics and efficacy in different clinical scenarios have been explored and increasingly clarified during its pre-marketing and post-marketing development. Nonetheless, numerous scientific and clinical issues remain not fully elucidated. This review discusses the pharmacodynamic and pharmacokinetic properties of trastuzumab and its current use in the treatment of breast cancer.